摘要:
7-amino-3-methoxymethyl-3-cephem-4-carboxylic acid of formula (I) can be easily prepared by reacting 7-aminocephalosporanic acid of formula (II) with an azeotropic mixture of trimethyl borate and methanol in the presence of methanesulfonic acid:
摘要:
The present invention relates to a pharmaceutical composition for treating or preventing obesity, comprising novel crystalline sibutramine methanesulfonate hemihydrate of formula (I). The crystalline sibutramine methanesulfonate hemihydrate according to the present invention has a much higher solubility in water, and enhanced stability under a high humidity/temperature condition, as compared with sibutramine hydrochloride monohydrate
摘要:
1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-α-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate.
摘要:
This invention relates to an improved method for stereoselectively preparing 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢¥-deoxy-2¢¥,2¢¥-difluorocytidine of formula (I).
摘要:
Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with removal of a silyl halide ((alkyl)3SiX (X=halide)); and deprotecting the nucleoside of formula (II) to obtain 2′-deoxy-2′,2′-difluorocytidine of formula (I). 2′-Deoxy-2′,2′-difluorocytidine of formula (I) is effective for treating various cancers such as non-small cell lung (NSCLC), pancreatic, bladder, breast or ovarian cancers.
摘要:
A flameproof thermoplastic resin composition is substantially free of phenolic resin, red phosphorous and silicone resin and comprises (A) about 40-95 parts by weight of a rubber modified styrene-containing resin comprising (a1) about 20-95% by weight of a styrene-containing graft copolymer resin containing about 19-50% by weight of acrylonitrile in the copolymer excluding rubber and (a2) about 5-80% by weight of a styrene-containing copolymer containing about 19-50% by weight of acrylonitrile; (B) about 5-60 parts by weight of a polyphenylene ether resin; (C) about 2-40 parts by weight of a compatabilizer comprising (c1) a styrene-containing copolymer containing about 5-18% by weight of acrylonitrile in the copolymer per 100 parts by weight of the sum of (A) and (B) or (c2) a styrene-containing graft copolymer having up to about 60% by weight of rubber wherein the compatabilizer contains about 5-18% by weight of acrylonitrile in the copolymer excluding rubber, per 100 parts by weight of the sum of (A) and (B); and (D) about 5-30 parts by weight of an aromatic phosphoric acid ester per 100 parts by weight of the sum of (A) and (B). The physical properties and flame retardance of the resin compositions according to the present invention are adversely affected by the presence of 3% or more by weight of polycarbonate based on the total weight of the composition.
摘要:
The present invention relates to a high-yield method for preparing highly pure (3S,4S)-4-((R)-2-(benzyloxy)tridecyl)-3-hexyl-2-oxetanone using a metal salt of (2S,3S,5R)-2-hexyl-3,5-dihydroxyhexadecanoic acid as an intermediate.
摘要:
Disclosed is (S)-(−)-amlodipine camsylate or a hydrate thereof having good photostability and high solubility, and a pharmaceutical composition comprising same, which can be efficiently used in treating cardiovascular diseases.
摘要:
Risperidone is prepared in a high yield by reacting 2,4-difluorophenyl(4-piperidinyl)methanone oxime hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in an aqueous alkali hydroxide solution having an alkali hydroxide concentration in the range of 20 to 40%.
摘要:
A flameproof thermoplastic resin composition substantially free of phenolic resin, red phosphorous and silicone resin comprises (A) about 40-95 parts by weight of a rubber modified styrene-containing graft copolymer resin, (B) about 5-60 parts by weight of polyphenylene ether resin; (C) about 5-30 parts by weight of aromatic phosphoric acid ester per 100 part by weight of (A) and (B) wherein the styrene-containing copolymer chains in rubber modified styrene-containing resin (A) comprise (i) about 5-20% by weight having an acrylonitrile fractionation content of 0-9% by weight (ii) about 10-40% by weight having an acrylonitrile fractionation content of 9-20% by weight and (iii) about 40-80% by weight having an acrylonitrile fractionation content of not less than 20% by weight acrylonitrile and the sum of (i), (ii), and (iii) is 100% by weight of the total weight of styrene-containing copolymer chains in rubber modified styrene-containing resin (A). The use of a rubber modified styrene-containing copolymer resin having a particular nitrile content distribution with polyphenylene ether resin to form a base resin and an aromatic phosphoric acid ester flame retardant produces resin compositions with high impact strength and flame retardancy. The compositions according to the present invention are substantially free of phenolic resin, red phosphorous, silicone resin and other components that are required by the prior art compositions containing polyphenylene ether resins and ABS type graft copolymers.